DE69921335T2 - CLEANER COMPONENTS CONTAINING AN ACTIVE SUBSTANCE AND A CATIONIC POLYMER - Google Patents

Abstract

A bar composition comprising a synthetic non-soap surfactant, a hydrophilic structurant, a water insoluble structurant, an oil/emollient benefit agent and a cationic polymer. The cationic polymer has a charge of density greater than 0.007 and is used in a specific ratio to the surfactant.

Description

The The present invention relates to bar-shaped compositions which capable of delivering active ingredients to the skin. More specifically the invention is based on pieces, the relatively large one Amounts of hydrophilic structurant (i.e. H. The relationship from hydrophilic to hydrophobic is at least 1: 2, preferably more than 40:60, more preferably at least 1 : 1 and strongest preferably over 1: 1) and in which it has been found that the cationic polymer, especially the cationic polymer with minimal level of charge density, unexpectedly enhances the deposition of the drug in these pieces.

Cationic polymers are well known in the art. Been For example in liquid cleansers, cationic hydrophilic polymers such as Polymer JR ^® from Americhol or Jaguar ^® by Rhone Poulenc, used to improve the delivery of drugs (such as in EP 93,602 ; WO 94/03152 and WO 94/03151).

cationic Polymers are also in bar-shaped formulations used. U.S. Patent No. 3,761,418 to Parran, Jr. teaches For example, a detergent composition (including soaps in piece form), containing water-insoluble, particulate Substances, such as antimicrobial agents and certain cationic ones Polymers to the deposition and retention of particulate substances to improve. Although soap formulations in piece form are used in the examples Become, the entire formulations are primarily soap and / or fatty acid structured. Furthermore not only are no active ingredients (oil / emollients) disclosed, but it would are also expected to be hydrophobic Structure improver the deposition of any oil / emollient would affect.

WHERE No. 95/26710 by Kacher et al. (transfer on P & G) a skin moisturizing and cleaning piece that is a skin cleanser and lipid moisturizer. Preferred optional ingredients are one or more cationic, polymeric skin conditioning agents that are added to a tactile feeling provide. However, the piece again becomes a rigid, crystalline network structure made up essentially of selected Fatty acid soap material consists. Applicants have found that this fatty acid soap material for the Deposition harmful is.

US Patent No. 5,425,892 to Taneri et al. teaches body cleansing freezers that a skeletal structure of neutralized carboxylic acid soap. The patent teaches polymeric skin feel aids, water-soluble organic compounds and oils. However, the pieces show As noted, a distinctive carboxylic acid structure different from the pieces of the invention, the relatively large Amounts of hydrophilic structural improver contains different.

Hydrophilic structured pieces themselves are taught as well, for example, in US Patent No. 5,520,840 by Massaro et al. or U.S. Patent No. 5,540,864 to Fair et al. However, there are no teachings regarding these in these references cationic polymers and no suggestion that these cationic compounds the separation of oil / emollients in pieces, the relatively large one Amounts of hydrophilic structural improver included, improve could. Furthermore There are no lessons or suggestions in this or any another reference to a critical relationship of cationic compound to surface-active Means, about the separation of oils / emollients is significantly improved, or that the cationic compounds must have a minimum level of charge density.

Finally teaches U.S. Patent No. 5,262,079 to Kacher et al. solid cleaning pieces with mild, neutral pH containing 5 to 50% by weight monocarboxylic fatty acids (the Provide skeletal structure), 20 to 65% bar-shaped strength aids and 15 to 55% water. The pieces may contain optional polyols (0 to 40%) as "chunky strength aids." The pieces are primarily fatty acid structured and the only piece-shaped strength aids, which are illustrated are isethionate (i.e., they have no minimal levels of hydrophilic z hydrophobic structurant on). Furthermore For example, the disclosed cationic compounds are guar, quaternized Guar, etc., all having a charge density of less than 0.007. It is therefore not apparent that only cationic polymers with a minimum charge activity for the purpose of the invention adequate are.

Suddenly and unexpectedly, Applicants discovered that cationic compounds, ie, cationic polymers having a minimum charge density level, can be used to control the deposition of oils / emollients into pieces comprising a relatively large amount of hydrophilic structurant (for example, the ratio of hydrophilic to hydrophilic) hydrophobic structural improvement with tel is at least 1: 2, preferably greater than 40:60, more preferably at least 1: 1, and most preferably greater than 1: 1; in addition, that the ratio of total soap and hydrophobic structurant to hydrophilic structurants does not exceed more than 10% by weight of the total composition), and that there is also a minimum critical ratio of cationic polymer to surfactant in which the deposition is noticeably improved. In addition, it is critical that the levels of surfactant, particularly the anionic compound, does not exceed certain ranges (so as not to affect deposition) and that minimal amounts of oil / emollient are used.

• (a) 10 bis 50 Gew.-%, vorzugsweise 20 bis 40 Gew.-% eines synthetischen, Nicht-Seife-, oberflächenaktiven Mittels, vorzugsweise eines anionischen oberflächenaktiven Mittels (beispielsweise Acylisethionat oder Alkalimetallaurylethersulfat);
• (b) 10 bis 40 Gew.-%, vorzugsweise 15 bis 35 Gew.-% eines hydrophilen Strukturverbesserungsmittels mit einem Schmelzpunkt zwischen 40 und 100°C (dieses Strukturverbesserungsmittel wird im allgemeinen eine Löslichkeit von mindestens 10% bei Raumtemperatur aufweisen);
• (c) 5 bis 20% eines wasserunlöslichen Strukturverbesserungsmittels mit einem Smp. zwischen 40 und 200°C;
• (d) 2 bis 40%, vorzugsweise 5 bis 20% Wirkstoff; und
• (e) 1,0% bis 10% kationisches Polymer;

wobei die Menge des unlöslichen Strukturverbesserungsmittels (c) und der Seife, wenn vorhanden, die Menge des hydrophilen Strukturverbesserungsmittels (b) um nicht mehr als 10 Gew.-% der gesamten stückförmigen Zusammensetzung übersteigt; wobei die Menge des kationischen Polymers (e) so ist, daß das Verhältnis der kationischen Verbindung zu dem oberflächenaktiven Mittel 0,06 : 1 bis 1 : 1, stärker bevorzugt 0,08 : 1 bis 0,5 : 1 beträgt; und wobei die Ladungsdichte des kationischen Polymers (Zahl von einwertigen Ladungen pro Wiederholungseinheit geteilt durch die Molmasse der Wiederholungseinheit) größer als 0,007 ist.More particularly, the subject invention relates to bar shaped compositions comprising:

• (a) 10 to 50%, preferably 20 to 40%, by weight of a synthetic non-soap surfactant, preferably an anionic surfactant (for example, acyl isethionate or alkali metal auryl ether sulfate);
• (b) 10 to 40%, preferably 15 to 35%, by weight of a hydrophilic structurant having a melting point between 40 and 100 ° C (this structurant will generally have a solubility of at least 10% at room temperature);
• (c) 5 to 20% of a water insoluble structurant having a m.p. between 40 and 200 ° C;
• (d) 2 to 40%, preferably 5 to 20% active ingredient; and
• (e) 1.0% to 10% cationic polymer;

wherein the amount of the insoluble structurant (c) and the soap, if present, exceeds the amount of the hydrophilic structurant (b) by not more than 10% by weight of the total bar composition; wherein the amount of the cationic polymer (e) is such that the ratio of the cationic compound to the surfactant is from 0.06: 1 to 1: 1, more preferably from 0.08: 1 to 0.5: 1; and wherein the charge density of the cationic polymer (number of monovalent charges per repeating unit divided by the molecular weight of the repeating unit) is greater than 0.007.

The Invention will now be described by way of example only with reference to the appended claims Drawing in which:

1 shows the deposition results as a function of the ratio of cationic compound to surfactant,
further described. As can be seen, the deposition increases significantly only when the ratio of the cationic compound to the surfactant reaches a certain minimum level.

The The present invention relates to relatively less active pieces (e.g. 50% active, preferably less than 40%, more preferably 30% and less active), wherein a relatively large Amount of hydrophilic structure improvers is present (hydrophobic Structure improvers and soap, if present, comprise not more than about 10% by weight more than the amount of hydrophilic Structure improvers), and also a relatively large amount on oil / emollient (i.e., at least 2%). Applicants discovered unexpectedly that if The relationship the cationic compound to the surfactant in these pieces is the same or over a certain defined relationship lies, the deposition of the active substance from the piece is noticeably improved. The cationic polymers used have to also have minimum defined levels of charge density.

The Piece becomes in more detail below described.

The pieces of the invention contain about 10 to 50 wt .-%, stronger preferably 15 to 40% by weight of a synthetic, non-soap, surface-active Agent. Suitable surface-active Agents are generally selected from the group consisting of anionic, nonionic, amphoteric, zwitterionic and / or cationic surfactants Means and mixtures thereof, selected as in the prior art is well known.

special becomes the surface active System generally at least one anionic surfactant Agent, a zwitterionic surfactant or preferably Mixtures of anionic or anionic and zwitterionic surface-active Means include.

The anionic surfactant which may be used may include aliphatic sulfonate such as a primary alkanesulfonate (e.g. C ₈ -C ₂₂ ), primary alkane disulfonate (e.g. C ₈ -C ₂₂ ), C ₈ -C ₂₂ alkene sulfonate, C ₈ -C ₂₂ -hydroxyalkanesulfonate or alkyl glyceryl ether sulfonate (AGS); or aromatic Sulfonates, such as alkylbenzene sulfonate.

The anionic compound may also be an alkyl sulfate (for example, C ₁₂ -C ₁₈ alkyl sulfate) or alkyl ether sulfate (including alkyl glyceryl ether sulfates). Among the alkyl ether sulfates are those having the formula: RO (CH ₂ CH ₂ O) _n SO ₃ M wherein R is an alkyl or alkenyl of 8 to 18 carbons, preferably 12 to 18 carbons, n has an average of greater than 1.0, preferably greater than 3; and M is a solubilizing cation, such as sodium, potassium, ammonium or substituted ammonium. Ammonium and sodium lauryl ether sulfates are preferred.

The anionic compound may also include alkyl sulfosuccinates (including mono- and dialkyl, for example C ₆ -C ₂₂ sulfosuccinates); Alkyl and acyl taurates, alkyl and acyl sarcosinates, sulfoacetates, C ₈ -C ₂₂ alkyl phosphates and phosphates, alkyl phosphate esters and alkoxylalkyl phosphate esters, acyl lactates, C ₈ -C ₂₂ monoalkyl succinates and maleates, sulfoacetates, alkyl glucosides and acyl isethionates.

Sulfosuccinates may be monoalkyl sulfosuccinates having the formula: R ¹ O ₂ CCH ₂ CH (SO ₃ M) CO ₂ M; and Amide MEA sulfosuccinates of the formula R ¹ CONHCH ₂ CH ₂ O ₂ CCH ₂ CH (SO ₃ M) CO ₂ M where R ^{1 is} between C ₈ -C ₂₂ alkyl and M is a solubilizing cation.

Sarcosinates are generally represented by the formula RCON (CH ₃ ) CH ₂ CO ₂ M wherein R is between C ₈ -C ₂₀ alkyl and M is a solubilizing cation.

Taurates are generally represented by the formula R ² CONR ³ CH ₂ CH ₂ SO ₃ M wherein R ^{2 is} C ₈ -C ₂₀ alkyl, R ^{3 is} C ₁ -C ₄ alkyl, and M is a solubilizing cation.

The C ₈ -C ₁₈ acyl isethionates are particularly preferred. These esters are prepared by the reaction between alkali metal isethionate with mixed aliphatic fatty acids having 6 to 18 carbon atoms and an iodine number of less than 20. At least 75% of the mixed fatty acids have 12 to 18 carbon atoms and up to 25% have 6 to 10 carbon atoms.

isethionates, when present, between about 10% to about 50% by weight of the entire piece-shaped composition lie. Preferably, this component is from about 20 to about 40% before.

The Acyl isethionate can be an alkoxylated isethionate, as in Ilardi et al., U.S. Patent No. 5,393,466, hereby incorporated by reference was described.

The anionic surfactant may also be a "soap". Under soap are alkali metal salts of aliphatic alkane- or alkene monocarboxylic acids, more generally known to be construed as C ₁₂ -C ₂₂ -Alkylfettsäuren. Sodium and potassium salts are preferred. A preferred soap is a mixture from about 15 to about 45% coconut oil and about 55 to about 85% tallow.

The Soaps can according to commercial acceptable standards of unsaturation contain. Excessive unsaturation is usually avoided.

The anionic component will be about 10 to 50% of the bar-shaped composition include.

entsprechen, wo R¹ Alkyl oder Alkenyl mit 7 bis 18 Kohlenstoffatomen ist; R² und R³ jeweils unabhängig voneinander Alkyl, Hydroxyalkyl oder Carboxyalkyl mit 1 bis 3 Kohlenstoffatomen ist; n 2 bis 4 ist; m 0 bis 1 ist; x Alkylen mit 1 bis 3 Kohlenstoffatomen ist, gegebenenfalls substituiert mit Hydroxyl, und y -CO₂ ^– oder -SO₃ ^– ist.Amphoteric detergents that may be used in this invention include min at least one acid group. This may be a carboxylic or a sulfonic acid group. They comprise quaternary nitrogen and are therefore quaternary amido acids. They should generally comprise an alkyl or alkenyl group of 7 to 18 carbon atoms. They are usually given a general structural formula:

where R ^{1 is} alkyl or alkenyl of 7 to 18 carbon atoms; R ² and R ^{3 are} each independently alkyl, hydroxyalkyl or carboxyalkyl of 1 to 3 carbon atoms; n is 2 to 4; m is 0 to 1; x is alkylene of 1 to 3 carbon atoms, optionally substituted with hydroxyl, and y is -CO ₂ ^- or -SO ₃ ^- .

und Amidobetaine der Formel:

wo m 2 oder 3 ist.Suitable amphoteric detergents within the above general formula include simple betaines of the formula:

and amidobetaines of the formula:

where m is 2 or 3.

In both formulas, R ^{1 is} alkyl or alkenyl of 7 to 18 carbons; and R ² and R ^{3 are} independently alkyl, hydroxyalkyl or carboxylalkyl of 1 to 3 carbons. R ¹ may in particular be a mixture of C ₁₂ and C ₁₄ alkyl groups derived from coconut so that at least half, preferably at least three quarters of the groups R ^{1 have from} 10 to 14 carbon atoms. R ² and R ³ are preferably methyl.

ist, wo m 2 oder 3 ist, oder Varianten von diesen, worin -(CH₂)₃SO₃ ^– durch

ersetzt wird.Another possibility is that the amphoteric detergent is a sulfobetaine of the formula:

where m is 2 or 3, or variants of these wherein - (CH ₂ ) ₃ SO ₃ ^-

is replaced.

In these formulas, R ¹ , R ² and R ^{3 are} as explained for amidobetaine.

The amphoteric compound generally 1 to 10% of the bar-shaped composition.

Other surfactants Agents (i.e., nonionic, cationic) may also optionally be used although not more than 0.01 to 20% by weight. the piece-shaped composition would include.

Nonionic surfactants include, in particular, the reaction products of compounds having a hydrophobic group and a reactive hydrogen atom, for example, aliphatic alcohols, acids, amides or alkylphenols with alkylene oxides, especially ethylene oxide either alone or with propylene oxide. Specific nonionic detergent compounds are alkyl (C ₆ -C ₂₂ ) phenol-ethylene oxide condensates, the condensation products of aliphatic, primary or secondary, linear or branched (C ₈ -C ₁₈ ) alcohols with ethylene oxide, and products formed by condensation of ethylene oxide were prepared with the reaction products of propylene oxide and ethylenediamine. Other so-called nonionic detergent compounds include long chain tertiary amine oxides, long chain tertiary phosphine oxides, and dialkyl sulfoxides.

The nonionic compound may also be a sugar amide, as well as a Polysaccharide amide. Specifically, the surfactant may be one of the Lactobionamides described in U.S. Patent No. 5,389,279 to Au et al., and polyhydroxyamides, as in U.S. Patent No. 5,312,954 to Letton et al.

Examples of cationic detergents are the quaternary ammonium compounds, such as alkyldimethylammonium halides.

Other surfactants Means that can be used are described in U.S. Patent No. 3,723,325 to Parran Jr. and "Surface Active Agents and Detergents "(Vol I & II) by Schwartz, Perry & Berch described.

A preferred composition at least 10% acyl isethionate and 1 to 10% betaine.

A another critical compound of the piece is the hydrophilic structure improver (For example, polyalkylene glycol).

These Component includes 10 to 40 wt .-%, preferably 15 to 35 wt .-% of the bar-shaped composition.

The Structure improver has a melting point of 40 to 100 ° C, preferably 45 to 100 ° C, stronger preferably 50 to 90 ° C on. In general, these structurants will become room temperature at least 10% water-soluble be.

Materials, as the water-soluble Structure improvers (b) are presented are polyalkylene oxides with reasonably high molecular weight of suitable melting point and in particular Polyethylene glycols or mixtures thereof.

polyethylene glycols (PEG's) that used can be have a molecular weight between 1,500 and 20,000.

It should be understood that (-8000 PEG), for example Carbowax ^® of Union Carbide () represents each product, a distribution of molecular weights (MW). Thus, for example, PEG 8,000 has an average MW between 7,000 and 9,000, while PEG 300 has an average MW between 285 and 315. The average MW of the product can be anywhere between the low and the low high value, and there may still be a good proportion of material with MW below the low value and above the high value.

In some embodiments of this invention, it is preferred to use a fairly small amount Polyalkylene glycol (for example, polyethylene glycol) having a molecular weight between 50,000 and 500,000, especially molecular weights 100,000 around. It has been found that these Polyethylene glycols improve the wear rate of the pieces. It is believed that this so, since their long polymer chains remain entangled themselves when the piece-shaped composition while the use is wetted.

If the high molecular weight polyethylene glycols (or any other water-soluble Polyalkylene oxides with high molecular weight) are used, the amount is preferably 1 to 5% by weight, stronger preferably 1 or 1.5 to 4 or 4.5% by weight of the composition. These materials are generally associated with a larger amount the other water-soluble Structure improver (b), such as the above-mentioned polyethylene glycol having a molecular weight of 1,500 to 10,000.

Some Polyethylene oxide-polypropylene oxide block copolymers melt at temperatures in the required range of 40 to 100 ° C and as part or whole of the water-soluble Structure improver (b) can be used. Here are block copolymers preferred in which polyethylene oxide at least 40 wt .-% of the block copolymer provides. These block copolymers may be blended with polyethylene glycol or other water-soluble Polyethylene glycol structurants are used.

In addition, can it is a mixture of lower and higher MW polyalkylene glycols as described in U.S. Patent No. 5,683,973 to Post et al. described.

It it should be noted that although not necessarily themselves are used, certain water-soluble auxiliary fillers along with the water-soluble Structure improvers can be used. Of these, for example Maltodextrin and the like water-soluble Strengthen included. If involved, these tools would not work more than about 10% by weight of the composition.

It is also required that the water Structure improvers have a melting point between 40 and 200 ° C, more preferably at least 50 ° C, especially 50 to 90 ° C exhibit. Suitable materials which are conceivable in particular are fatty acids, especially those with a carbon chain of 12 to 24 carbon atoms. Examples are lauric, myristic, palmitic, stearic, arachidonic and behenic acids and mixtures thereof. Sources of these fatty acids are coconut, topped Coconut-, Palm, palm kernel, babassu and tallow fatty acids and partially or fully hydrogenated fatty acids or distilled fatty acids. Other suitable, water-insoluble Structure improvers include alkanols of 8 to 20 carbon atoms, especially cetyl alcohol. These materials generally have a water solubility less than 5 g / liter at 20 ° C on.

The relative proportions of water-soluble Structure improvers and water insoluble structurants determine the speed at which the piece moves during the Use wears off. The presence of the water insoluble structurant delayed usually the resolution of the piece, if it's during the use is exposed to the water, and therefore delays the Wear rate.

in the general becomes insoluble Structure improver 5 to 20% by weight of the composition include.

Exceeds according to the invention the amount of water insoluble Structure improver (c) not the amount of hydrophilic Structure improver (b) plus any soap that may be present by more than about 10% by weight. While not wished is bound to be bound by a theory, it is believed that if there is too much soap and / or hydrophilic structure improver, the deposition level is reduced.

The active ingredient of the compositions of the invention is included in the compositions to moisturize, condition and / or protect the skin. By "active ingredient" is meant a substance that softens the skin (horny layer of the skin) and retards it by delaying Reducing their water content softens and / or protects the skin.

• (a) Silikonöle, Gummis und Modifikationen davon, wie lineare und cyclische Polydimethylsiloxane, Amino-, Alkyl-, Alkylaryl- und Arylsilikonöle;
• (b) Fette und Öle, einschließlich natürliche Fette und Öle, wie Jojoba-, Sojabohnen-, Sonnenblumen-, Reiskleie-, Avocado-, Mandel-, Oliven-, Sesam-, Pfirsichkern-, Rizinus-, Kokosnuß-, Nerzöle; Kakaofett, Rindertalg, Schweinefett; gehärtete Öle, erhalten durch Hydrieren der zuvor genannten Öle; und synthetische Mono-, Di- und Triglyceride, wie Myristinsäureglycerid und 2-Ethylhexansäureglycerid;
• (c) Wachse, wie Karnaubawachs, Walrat, Bienenwachs, Lanonin und Derivate davon;
• (d) hydrophobe Pflanzenextrakte;
• (e) Kohlenwasserstoffe, wie flüssige Paraffine, Vaseline, mikrokristallines Wachs, Ceresin, Squalen, Squalan und Mineralöl;
• (f) höhere Fettsäuren, wie Laurin-, Myristin-, Palmitin-, Stearin-, Behen-, Öl-, Leinöl-, Lanolin-, Isostearinsäuren und polyungesättigte Fettsäuren (PUFA);
• (g) höherer Alkohole, wie Lauryl-, Cetyl-, Steryl-, Oleyl-, Behenyl-, Cholesterol- und 2-Hexadecanolalkohol;
• (h) Ester, wie Cetyloctanoat, Myristyllactat, Cetyllactat, Isopropylmyristat, Myristylmyristat, Isopropylpalmitat, Isopropyladipat, Butylstearat, Decyloleat, Cholesterolisostearat, Glycerolmonostearat, Glyceroldistearat, Glyceroltristearat, Alkyllactat (beispielsweise Lauryllactat), Alkylcitrat und Alkyltartrat;
• (i) wichtige Öle, wie Fischöle, Mentha-, Jasmin-, Kampher-, Weißzedern-, Pomeranzenschalen-, Ryu-, Terpentin-, Zimt-, Bergamott-, Citrus unshiu-, Kalmus-, Kiefern-, Lavendel-, Lorbeer-, Gewürznelken-, Hiba-, Eukalytpus-, Zitronen-, Sternblumen-, Thymian-, Pfefferminz-, Rosen-, Salbei-, Menthol-, Cineol-, Eugenol-, Citral-, Citronell-, Borneol-, Linalool-, Geraniol-, Nachtkerzen-, Kampher-, Thymol-, Spirantol-, Pinen-, Limonen- und Terpenoidöle;
• (j) Lipide, wie Cholesterol, Ceramide, Saccharoseester und Pseudo-Ceramide, wie in der europäischen Patentanmeldung Nr. 556,957 beschrieben;
• (k) Vitamine, wie Vitamin A und E, und Vitaminalkylester, einschließlich den Vitamin-C-Alkylestern;
• (l) Sonnenschutzmittel, wie Octylmethoxylcinnamat (Parsol MCX) und Butylmethoxybenzoylmethan (Parsol 1789);
• (m) Phospholipide;
• (n) Feuchthaltemittel, wie Glycerin, Propylenglykol und Sorbitol; und
• (o) Gemische aus irgendwelchen der vorhergehenden Komponenten.

Preferred active ingredients include:

• (a) silicone oils, gums and modifications thereof, such as linear and cyclic polydimethylsiloxanes, amino, alkyl, alkylaryl and aryl silicone oils;
• (b) fats and oils, including natural fats and oils, such as jojoba, soybean, sunflower, rice bran, avocado, almond, olive, sesame, peach, castor, coconut, mink oils; Cocoa fat, beef tallow, pork fat; hardened oils obtained by hydrogenating the aforementioned oils; and synthetic mono-, di- and triglycerides such as myristic acid glyceride and 2-ethylhexanoic acid glyceride;
• (c) waxes such as carnauba wax, spermaceti, beeswax, lanonin and derivatives thereof;
• (d) hydrophobic plant extracts;
• (e) hydrocarbons, such as liquid paraffins, vaseline, microcrystalline wax, ceresin, squalene, squalane and mineral oil;
• (f) higher fatty acids, such as lauric, myristic, palmitic, stearic, beehive, oleic, linseed, lanolin, isostearic and polyunsaturated fatty acids (PUFA);
• (g) higher alcohols, such as lauryl, cetyl, steryl, oleyl, behenyl, cholesterol and 2-hexadecanol alcohols;
• (h) esters such as cetyl octanoate, myristyl lactate, cetyl lactate, isopropyl myristate, myristyl myristate, isopropyl palmitate, isopropyl adipate, butyl stearate, decyl oleate, cholesterol stearate, glycerol monostearate, glycerol distearate, glycerol tristearate, alkyl lactate (e.g., lauryl lactate), alkyl citrate, and alkyl tartrate;
• (i) important oils such as fish oils, mentha, jasmine, camphor, white celery, bitter orange peel, ryu, turpentine, cinnamon, bergamot, citrus unshiu, calamus, pine, lavender, laurel , Clove, hiba, eucalyptus, citric, star flower, thyme, peppermint, rose, sage, menthol, cineole, eugenol, citral, citronell, borneol, linalool, Geraniol, evening primrose, camphor, thymol, spirant, pinene, limonene and terpenoid oils;
• (j) lipids such as cholesterol, ceramides, sucrose esters and pseudo-ceramides as described in European Patent Application No. 556,957;
• (k) vitamins, such as vitamins A and E, and vitamin C esters, including the vitamin C alkyl esters;
• (l) sunscreen agents such as octyl methoxyl cinnamate (Parsol MCX) and butyl methoxybenzoylmethane (Parsol 1789);
• (m) phospholipids;
• (n) humectants, such as glycerine, propylene glycol and sorbitol; and
• (o) mixtures of any of the foregoing components.

Where adverse interactions between the drug and surfactant Fabric usually are particularly acute, the active ingredient in the compositions of the invention be introduced in a carrier.

These Active ingredients include lipids; alkyl lactates; Sunscreen; esters, such as isopropyl palmitate and isopropyl myristate; and vitamins. The carrier can For example, be a silicone or hydrocarbon oil, the not by the surface active Phase soluble is made / micelles and in which the active ingredient is relatively soluble.

Especially preferred agents include silicone oils, gums, and modifications thereof, esters such as isopropyl palmitate and myristate and alkyl lactates, and vegetable oils, like sunflower oil.

Of the Active ingredient can be provided in the form of an emulsion.

Of the Active ingredient used in the invention may also be used as A carrier act to deliver the active agents to the skin, the with the compositions according to the invention was treated. This approach is particularly useful for delivering the effective agents, which are difficult to deposit on the skin, or those under harmful Interactions with other components in the composition Suffer. In these cases is the carrier often a silicone or hydrocarbon oil, not by the surface-active Phase soluble is made / micelles and in which the active ingredient is relatively soluble. Examples these active agents include antiviral agents; Hydroxycaprylsäuren; pyrrolidone; Carboxylic acids; 3,4,4'-trichlorocarbanilide; benzoyl peroxide; Fragrances; essential oils; germicides and insect repellents, such as 2,4,4'-trichloro-2'-hydroxydiphenyl ether (Irgasan DP300); salicylic acid; Willow extract, N, N-dimethyl-m-toluamide (DEET); and mixtures thereof.

Of the Active ingredient From 2 to 40% by weight, preferably from 5 to 20% by weight of the composition.

Finally is the cationic polymer (deposition aid) is a water-soluble cationic polymer or copolymers having a molecular weight from about 1,000 to 2,000,000 and a higher cationic charge density. Specifically, the cationic charge density should be at least 0.007 and be more, where the cationic charge density as the number of monovalent Charges per repeating unit divided by the molecular weight of the Repeat unit is defined.

Therefore, for example, a cationic compound of the Jaguar ^® type, such as Jaguar C14S ^® (as in the example et RR of Kacher al. US-A-5,262,079 used), a charge density of 0.0008 to under the threshold value of the invention as [ N - [- 3- (dimethylammonio) propyl] urea dichloride] (Mirapol A15 ^®) having a charge density of 0.00661. In contrast, dimethyldiallylammonium chloride (Merquat 100 ^®) a density of 0.00793 and is within the invention.

It is also for the cationic polymer is important, (a) prior to incorporation into the bar formulation and (b) at a concentration of 1% by weight or more for the desired one Benefit, d. H. improved deposition to be fully hydrated. The commercial application (usability) of the invention would therefore require that cationic polymer is present at a relatively high concentration, when it is hydrated, the impracticability, difficulty and impossibility high cost of drying the bar detergent formulation to avoid. A cationic polymer such as dimethyldiallylammonium chloride (Brand name Merquat 100) can be used at concentrations of 40% (60% water) be prepared while the quaternary cationic guar polymer with low charge density (trade name Jaguar C14S), exemplified by Kacher et al., At concentrations only of about 3% (97% water) can be produced and not commercially is practical.

Exemplary cationic polymers of the invention can be used invention include Salcare type polymers from Allied Colloids ^® type, and Merquat type polymers from Calgon ^® type.

These cationic polymers of the invention are not generally applicable to the invention are the polymers having a high molecular weight, low charge density, such as Polymer JR-400 ^® from Amerchol and cationic polysaccharides of the class of the cationic guar gums such as Jaguar C14S ^® from Rhone-Poulenc.

It is an important aspect of the invention that it has a minimal amount of to be used cationic polymer. The ratio of cationic compound to the surfactant is 0.06 : 1 to 1: 1, stronger preferably 0.08: 1 to 0.5: 1.

In addition, should The relationship of the hydrophilic structurant to the total soap and hydrophobic structurant at least 1: 2, preferably 40: 40, stronger preferably at least 1: 1, and most preferably more than 1 : 1 amount.

To to the operating and comparative examples or where otherwise expressly stated, it is understood that all Numbers in this description, the quantities and ratios of the material or reaction conditions, physical properties indicate the materials and / or use modified by the word "about".

If Furthermore as used in the specification and claims, it is so understand that expression comprises or comprising the presence of said features, integers, Indicates steps, components, etc., but the presence or supplement of one or more features, integers, steps, components or groups of them does not exclude.

The The following examples are intended to further explain the invention and should the claims by no means restrict.

Examples

materials and procedures

materials

Sodium cocoyl isethionate was supplied by Lever Baltimore, polyethylene glycol (PEG 8000) was supplied by Union Carbide, and Merquat 100 (cationic polymer) was supplied by Calgon Corporation. Polydimethylsiloxane (PDMS) with a viscosity of 60,000 cs was from Dow Corning, maltodextrin was from Grain Processing Corp., and the cocoamidopropyl betaine was from Goldschmidt. Palmitic, steric acid and sodium stearate were supplied by Unichema.

In vivo measurements Deposition

Fourier transform infrared spectroscopy with weakened Total Reflection (ATR-FTIR) was the analytical technique used to to measure the silicone deposition. The standard procedure is below documented.

formulation processing

The piece-shaped formulations were made in a 2 liter Patterson mixer. The fatty acid and Sodium stearate was at 90 ° C mixed together. Cocoyl isethionate was then added, followed of betaine and the minor ingredients. After mixing for thirty minutes and dry to about 7% water was added to a polyethylene glycol and maltodextrin. This was for mixed for another ten minutes. The cover was removed and the silicone and Merquat 100 were added. The moisture content was by Karl Fisher titration with a turbo titration device certainly.

at the final one Moisture level (~ 5%) was the formulation on a heated applicator roll dripped and then became over a chill roll dismembered. The cooling roll splitter were in a Weber-Seelander twin mill with a screw speed at ~ 20 U / min extruded.

The The tip of the extruder was heated to 45 to 50 ° C. The cut blocks were using a Weber-Seelander-L4 hydraulic press with a kissenförmgen Nylon nozzle immediately pressed.

The inclusion of the drug (for example, polydimethylsiloxane) -like in Dove ^® compositions (for example Hochacylisethionatstücke structured with fatty acid) or primarily soap-based composition results in negligible deposition of the active ingredient. High levels of surfactant (e.g., 60%) and insoluble structurants (e.g., fatty acid) generally inhibit transfer of the drug to the skin. Even the addition of less active, hydrophilic, structured pieces such as those disclosed in U.S. Patent No. 5,520,840 to Massaro et al. be taught leads to little deposition. However, in order to study the effect of the cationic polymer in these low-activity, hydrophilic structural enhancement agent pieces, the following compositions were prepared.

Table 1

In general, the compositions were prepared by mixing ingredients at a temperature sufficiently high to provide a mixture, cooling on a chill roll to form chips / flakes, extruding, cutting and pressing. The produced compositions who those shown in Table 1 above.

The attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR) was the analytical technique used to measure the silicon deposition. In the standard procedure, the test piece is wetted and rotated ten times in the hand, then the inner forearm is wetted and the piece is rubbed on the forearm ten times. This is followed by a thirty second wash and a fifteen second rinse. The arm is then dried and an infrared scan of the inner forearm is obtained. The silicone is quantified by integrating the absorption band between 770 cm ^-1 and 835 cm ^-1 . This is entered on a standard curve and the deposition value in μg / cm ² indicated.

The deposition results of the experimentally designed formulations are summarized in Table 2 and described in 1 shown graphically. The observed wide variance is due to different skin types and skin conditions, which requires a minimum of about 8 independent measurements per prototype.

Table 2: In vivo deposition of the experimentally constructed pieces

As As can be seen, the amount of oil deposited on the skin a function of the relationship from cationic polymer to surfactant. Specifically, a minimum ratio of 0.06 seems necessary to be. In the absence of the polymer optically no silicone on the skin from the piece-shaped prototypes demonstrated. If the ratio Polymer to surfactant Medium increased will be a considerable increase observed the deposition.

The The following formulations were selected for further deposition.

For example 6 is the ratio cationic compound / surfactant Mean = 0.083.

For example 7 is the ratio cationic compound / surfactant Mean = 0.0625.

example 6 contained 30% sodium cocoyl isethionate (SCI) with 2.5% Merquat and 10% PDMS. In the example, the SCI was increased to 40%. The Merquat and PDMS levels were not changed.

The Deposition results from the formulations are shown below Table 4 shows:

Table 4

table 4 also compares the in-vivo deposition of the piece-shaped prototypes (Examples 6 & 7) with a liquid Body wash (example 8th). As noted, significantly higher levels of oil on the Skin from the piece-shaped prototypes deposited.

Claims (11)

Piece-shaped composition, full: (a) 10 to 50% by weight of synthetic, non-soap, surfactant Medium, selected from the group consisting of anionic, nonionic, cationic, amphoteric / zwitterionic surfactants and mixtures from that; (b) 10 to 40% by weight of a hydrophilic structure improver with a melting point between 40 and 100 ° C; (c) 5 to 20% by weight a water-insoluble Structure improver having a melting point of 40 to 200 ° C; (D) 2 to 40% of an active ingredient, which softens the skin and by delaying her softens the depletion of its water content and / or protects the skin; (E) 1.0 to 10% by weight of cationic polymer having a molecular weight from 1000 to 2,000,000 daltons; being the amount of insoluble Structure improver (c) and soap, if any, the amount of the hydrophilic structure improver (b) is not exceeds 10% by weight of the total bar-shaped composition; and wherein the amount of the cationic polymer (e) is such that the ratio of the cationic polymer to the surfactant 0.06: 1 to 1: 1; and wherein the charge density of the cationic polymer is greater than 0.007, and where the ratio of the hydrophilic to hydrophobic structure improver at least 1: 2. A composition according to claim 1, wherein the surfactant An anionic surfactant Means is. A composition according to claim 2, wherein the surfactant Average is acyl isethionate or alkali metal alkyl ether sulfate. A composition according to any one of the preceding claims, comprising 15 to 40% by weight (a). A composition according to any one of the preceding claims, comprising 15 to 35% by weight (b). A composition according to any one of the preceding claims, wherein the hydrophilic structure improver (b) at room temperature at least 10% water-soluble is. A composition according to any one of the preceding claims, wherein the hydrophilic structural improver (b) of polyalkylene oxides MW 1500 to 20,000 and block copolymers of polyethylene and polypropylene oxide and mixtures thereof is. A composition according to any one of the preceding claims, wherein the insoluble structurant (c) is C ₁₂ to C ₂₄ fatty acid. A composition according to any one of the preceding claims, wherein the active ingredient (d) comprises 5 to 20% by weight of the composition. A composition according to any one of the preceding claims, comprising 1.0% to 7% cationic polymer. A composition according to any one of the preceding claims, wherein The relationship of the cationic polymer to the surfactant in the range from 0.08: 1 to 0.5: 1.